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从越南四角风车子中分离得到的α-葡萄糖苷酶抑制性环阿尔廷烷类化合物

α-Glucosidase Inhibitory Cycloartanes from the Vietnamese Combretum quadrangulare.

作者信息

Nguyen Huu-Hung, Duong Thuc-Huy, Truong Nguyen Huy, Vo Thanh-Sang, Mai Dinh-Tri, Nguyen Thi Thuong Huyen, Bui Xuan-Hao, Nguyen Ngoc-Hong, Do Thi-Hong-Tuoi

机构信息

Faculty of Applied Technology, School of Engineering and Technology, Van Lang University, Ho Chi Minh City, 700000, Vietnam.

Department of Chemistry, Ho Chi Minh City University of Education, 280 An Duong Vuong Street, District 5, Ho Chi Minh City, 748342, Vietnam.

出版信息

Chem Biodivers. 2022 Oct;19(10):e202200562. doi: 10.1002/cbdv.202200562. Epub 2022 Sep 23.

Abstract

Leaves of Combretum quadrangulare Kurz showed potent α-glucosidase inhibition. Two new cycloartane-type triterpenes, combretic acids D and E were isolated from the bioactive fraction. The chemical structures were determined using NMR and MS methods. Combretic acid D represents for the first cycloartane having a dihydrofuran ring in the side chain. Combretic acids D and E showed significant α-glucosidase inhibition, with IC values of 13.9 and 30.7 μM, respectively. Combretic acid D was determined to be a non-competitive type in the kinetic study. The docking study in combination with dynamic simulations of this compound provided the molecular understanding of α-glucosidase inhibition.

摘要

四角风车子(Combretum quadrangulare Kurz)的叶子表现出较强的α-葡萄糖苷酶抑制活性。从其生物活性部位分离得到了两种新的环阿尔廷烷型三萜类化合物——风车子酸D和风车子酸E。通过核磁共振(NMR)和质谱(MS)方法确定了它们的化学结构。风车子酸D是首个侧链含有二氢呋喃环的环阿尔廷烷。风车子酸D和风车子酸E均表现出显著的α-葡萄糖苷酶抑制活性,其半数抑制浓度(IC)值分别为13.9 μM和30.7 μM。在动力学研究中,风车子酸D被确定为非竞争性类型。该化合物的对接研究结合动力学模拟为α-葡萄糖苷酶抑制作用提供了分子层面的理解。

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